trastuzumab emtansine

**Trastuzumab emtansine** is a HER2-directed antibody-drug conjugate composed of the humanized anti-HER2 IgG1 monoclonal antibody trastuzumab covalently linked through a stable noncleavable thioether MCC linker to DM1, a maytansinoid microtubule inhibitor. Following HER2 binding and receptor-mediated internalization, lysosomal degradation releases DM1-containing catabolites that disrupt microtubule dynamics, cause cell-cycle arrest, and promote apoptosis in HER2-expressing tumor cells. The trastuzumab component also retains HER2-targeting and signaling-inhibitory activity. Marketed as Kadcyla, it was developed by Genentech and Roche with DM1 technology originating from ImmunoGen, and is approved for selected HER2-positive metastatic and early breast cancer settings.

Brand names

Kadcyla

Other names

ado-trastuzumab emtansinetrastuzumab-DM1trastuzumab-DM-1trastuzumab-DM 1trastuzumab-MCC-DM1trastuzumab-MCC-DM-1trastuzumab-MCC-DM 1